Xiquan Zhang,Aiming Zhang,Zhou Zhou,Leilei Yang,Huadong Yao,Xueyan Zhu,Hubo Wang
申请号：
US16066482
公开号：
US10562904B2
申请日:
2016.12.29
申请国别(地区):
US
年份:
2020
代理人:
摘要：
The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production.
